Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.

Abstract A series of 4′-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives ( Ia–Il ) were synthesized and biologically evaluated. It was found that Ig , the most active compound, antagonized both Ang II AT 1 and endothelin ET A receptors (AT 1 IC 50  = 8.5, ET A IC 50  = 8.9 nM), and was more potent than losartan in RHRs with no significant effect on heart rate. The preliminary structure–activity relationships were also discussed in the present paper.